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WO2005002552A3 - Benzimidazole derivatives and their use as protein kinases inhibitors - Google Patents

Benzimidazole derivatives and their use as protein kinases inhibitors Download PDF

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Publication number
WO2005002552A3
WO2005002552A3 PCT/GB2004/002824 GB2004002824W WO2005002552A3 WO 2005002552 A3 WO2005002552 A3 WO 2005002552A3 GB 2004002824 W GB2004002824 W GB 2004002824W WO 2005002552 A3 WO2005002552 A3 WO 2005002552A3
Authority
WO
WIPO (PCT)
Prior art keywords
protein kinases
benzimidazole derivatives
kinases inhibitors
compounds
kinases
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/GB2004/002824
Other languages
French (fr)
Other versions
WO2005002552A2 (en
Inventor
Valerio Berdini
Michael Alistair O'brien
Maria Grazia Carr
Theresa Rachel Early
Eva Figueroa Navarro
Adrian Liam Gill
Steven Howard
Gary Trewartha
Alison Jo-Anne Woolford
Andrew James Woodhead
Paul Wyatt
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Astex Technology Ltd
Original Assignee
Astex Technology Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB0315657.7A external-priority patent/GB0315657D0/en
Priority claimed from GB0324919A external-priority patent/GB0324919D0/en
Priority to KR1020067000119A priority Critical patent/KR101190964B1/en
Priority to US10/564,166 priority patent/US7977477B2/en
Priority to DK04743172.1T priority patent/DK1648426T3/en
Priority to SI200432125T priority patent/SI1648426T1/en
Priority to JP2006518329A priority patent/JP4833059B2/en
Priority to AU2004253338A priority patent/AU2004253338B2/en
Priority to CA2531050A priority patent/CA2531050C/en
Priority to ES04743172.1T priority patent/ES2443995T3/en
Priority to EP04743172.1A priority patent/EP1648426B1/en
Priority to NZ543959A priority patent/NZ543959A/en
Priority to CN2004800249288A priority patent/CN1845734B/en
Application filed by Astex Technology Ltd filed Critical Astex Technology Ltd
Priority to HK06108214.7A priority patent/HK1087925B/en
Priority to MXPA05014223A priority patent/MXPA05014223A/en
Priority to PL04743172T priority patent/PL1648426T3/en
Publication of WO2005002552A2 publication Critical patent/WO2005002552A2/en
Publication of WO2005002552A3 publication Critical patent/WO2005002552A3/en
Priority to IL172840A priority patent/IL172840A/en
Anticipated expiration legal-status Critical
Priority to US13/116,121 priority patent/US20110224203A1/en
Priority to US13/902,325 priority patent/US20140010892A1/en
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The invention provides compounds having activity as inhibitors of cyclin dependent kinases, glycogen synthase kinase-3 and Aurora kinases for use in the treatment of disease states and conditions such as cancer that are mediated by the kinases. The compounds have the general formula (I). Also included within formula (I) are the salts, solvates and N-oxides of the compounds.
PCT/GB2004/002824 2003-07-03 2004-07-05 Benzimidazole derivatives and their use as protein kinases inhibitors Ceased WO2005002552A2 (en)

Priority Applications (17)

Application Number Priority Date Filing Date Title
MXPA05014223A MXPA05014223A (en) 2003-07-03 2004-07-05 Benzimidazole derivatives and their use as protein kinases inhibitors.
PL04743172T PL1648426T3 (en) 2003-07-03 2004-07-05 Benzimidazole derivatives and their use as protein kinases inhibitors
CN2004800249288A CN1845734B (en) 2003-07-03 2004-07-05 Benzimidazole derivatives and their use as protein kinases inhibitors
DK04743172.1T DK1648426T3 (en) 2003-07-03 2004-07-05 BENZIMIDAZOLD DERIVATIVES AND USE THEREOF AS PROTEINKINASE INHIBITORS
SI200432125T SI1648426T1 (en) 2003-07-03 2004-07-05 Benzimidazole derivatives and their use as protein kinases inhibitors
JP2006518329A JP4833059B2 (en) 2003-07-03 2004-07-05 Pharmaceutical compounds
AU2004253338A AU2004253338B2 (en) 2003-07-03 2004-07-05 Benzimidazole derivatives and their use as protein kinases inhibitors
CA2531050A CA2531050C (en) 2003-07-03 2004-07-05 Pharmaceutical compounds
ES04743172.1T ES2443995T3 (en) 2003-07-03 2004-07-05 Benzimidazole derivatives and their uses as protein kinase inhibitors
EP04743172.1A EP1648426B1 (en) 2003-07-03 2004-07-05 Benzimidazole derivatives and their use as protein kinases inhibitors
HK06108214.7A HK1087925B (en) 2003-07-03 2004-07-05 Benzimidazole derivatives and their use as protein kinases inhibitors
KR1020067000119A KR101190964B1 (en) 2003-07-03 2004-07-05 Benzimidazole derivatives and their use as protein kinases inhibitors
US10/564,166 US7977477B2 (en) 2003-07-03 2004-07-05 Benzimidazole derivatives and their use as protein kinase inhibitors
NZ543959A NZ543959A (en) 2003-07-03 2004-07-05 Benzimidazole derivatives and their use as protein kinase inhibitors
IL172840A IL172840A (en) 2003-07-03 2005-12-27 Benzimidazole derivatives and their use as protein kinase inhibitors
US13/116,121 US20110224203A1 (en) 2003-07-03 2011-05-26 Benzimidazole derivatives and their use as protein kinase inhibitors
US13/902,325 US20140010892A1 (en) 2003-07-03 2013-05-24 Benzimidazole derivatives and their use as protein kinase inhibitors

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US48468503P 2003-07-03 2003-07-03
US60/484,685 2003-07-03
GB0315657.7 2003-07-03
GBGB0315657.7A GB0315657D0 (en) 2003-07-03 2003-07-03 Pharmaceutical compounds
US51437403P 2003-10-24 2003-10-24
US60/514,374 2003-10-24
GB0324919A GB0324919D0 (en) 2003-10-24 2003-10-24 Pharmaceutical compounds
GB0324919.0 2003-10-24

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US13/116,121 Division US20110224203A1 (en) 2003-07-03 2011-05-26 Benzimidazole derivatives and their use as protein kinase inhibitors

Publications (2)

Publication Number Publication Date
WO2005002552A2 WO2005002552A2 (en) 2005-01-13
WO2005002552A3 true WO2005002552A3 (en) 2005-06-16

Family

ID=46045485

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2004/002824 Ceased WO2005002552A2 (en) 2003-07-03 2004-07-05 Benzimidazole derivatives and their use as protein kinases inhibitors

Country Status (15)

Country Link
US (3) US7977477B2 (en)
EP (2) EP1648426B1 (en)
JP (1) JP4833059B2 (en)
CN (1) CN1845734B (en)
AU (1) AU2004253338B2 (en)
CA (1) CA2531050C (en)
DK (2) DK2305250T3 (en)
ES (2) ES2443995T3 (en)
MX (1) MXPA05014223A (en)
NZ (1) NZ543959A (en)
PL (2) PL1648426T3 (en)
PT (2) PT2305250E (en)
SI (2) SI2305250T1 (en)
TW (1) TWI372050B (en)
WO (1) WO2005002552A2 (en)

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US9346815B2 (en) 2014-05-23 2016-05-24 Genentech, Inc. 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds, compositions and methods of use thereof
US10307426B2 (en) 2017-05-22 2019-06-04 Genentech, Inc. Therapeutic compounds and compositions, and methods of use thereof
US11649241B2 (en) 2017-03-14 2023-05-16 Genentech, Inc. Pyrazolochlorophenyl compounds, compositions and methods of use thereof

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* Cited by examiner, † Cited by third party
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US9346815B2 (en) 2014-05-23 2016-05-24 Genentech, Inc. 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds, compositions and methods of use thereof
US9604984B2 (en) 2014-05-23 2017-03-28 Genentech, Inc. 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds, compositions and methods of use thereof
US11649241B2 (en) 2017-03-14 2023-05-16 Genentech, Inc. Pyrazolochlorophenyl compounds, compositions and methods of use thereof
US10307426B2 (en) 2017-05-22 2019-06-04 Genentech, Inc. Therapeutic compounds and compositions, and methods of use thereof

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